Pracinostat (SB939)

製品コードS1515

Pracinostat (SB939)化学構造

分子量(MW):358.48

Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.

サイズ 価格(税別)  
JPY 49800.00
JPY 34860.00
JPY 61420.00
JPY 144420.00

カスタマーフィードバック(5)

  • A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells.

    Oncotarget, 2016, 7(23):34384-94. Pracinostat (SB939) purchased from Selleck.

    Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.

    Antimicrob Agents Chemother 2012 56(7), 3849-56. Pracinostat (SB939) purchased from Selleck.

  • (B) Immunoblots showing induction of apoptosis in K562 BIMi2+/+, BIMi2+/- and BIMi2-/-. The data shown are representative of 3 experiments with similar results. Cells were treated for 48hours with SB939 at the indicated concentrations. p-BCR-ABL, phosphorylated BCR-ABL; STAT5, signal transducer and activator of transcription 5; p-STAT5, phosphorylated STAT5; BIMEL, BIM extra long isoform; BIML, BIM long isoform; Cl. CASP3, cleaved CASPASE3; Cl. PARP, cleaved PARP. 48-hour treatment as in A.

    PLoS One, 2017, 12(3):e0174107. Pracinostat (SB939) purchased from Selleck.

    A: Mean fold change in γ-globin mRNA in erythroid progenitor cells treated with the designated therapeutic candidates (MS-275, SDMB, SB939, or Benserazide), compared to vehicle-treated cells from the same subject. All changes are significant, p <0.001. Error bars indicate SD. B. Mean change in proportions of cells expressing HbF protein (F-reticulocytes) in erythroid progenitor cells treated with therapeutic candidates (SDMB, Benserazide, MS275, SB939), compared to control cells from the same subject. Error bars indicate SD. * Asterisks indicate statistically significant differences (* p<0.05, ** p<0.01. *** p<0.001)

    Blood Cells Mol Dis, 2016, 56(1):62-9. Pracinostat (SB939) purchased from Selleck.

  • Breast cancer cells were treated with the indicated concentrations of SB939.

     

     

    Dr. Zhang of Tianjin Medical University. Pracinostat (SB939) purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.
特性 A new histone deacetylase inhibitor based on hydroxamic acid, with improved physicochemical, pharmaceutical, and pharmacokinetic properties.
ターゲット
HDAC10 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC5 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC4 [1]
(Cell-free assay)
40 nM 43 nM 47 nM 49 nM 56 nM
体外試験

SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. SB939 is a potent inhibitor of HDAC class I isoenzymes, HDAC1, HDAC2, HDAC3 and HDAC8 with the IC50 values ranging from 43 nM to 140 nM. SB939 inhibits HDAC class II isoenzymes , HDAC4, HDAC5, HDAC7, HDAC9 and HDAC10 significantly with the IC50 values ranging from 40 nM to 137 nM, with the exception of HDAC6 which shows IC50 of 1008 nM. It markedly inhibits HDAC11 of the HDAC class IV enzymes with IC50 of 93 nM, but shows no inhibitory activity against SIRT 1 of the class III HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, especially Leukemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells). [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells MonUVJJwdGmoZYLheIlwdiCjc4PhfS=> NHvMW2k1QCCq NGnOSINCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE4yPyEQvF2= Ml7RNlQyOTl3NUW=
NCI-H460 cells NIPsVnFRem:uaX\ldoF1cW:wIHHzd4F6 MVu0PEBp M1rmdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC5{MjFOwG0> MXGyOFEyQTV3NR?=
HCT116 cells Mm\MVJJwdGmoZYLheIlwdiCjc4PhfS=> NYT0XYpXPDhiaB?= NX65dFFGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC5{NDFOwG0> MljsNlQyOTl3NUW=
MDA-MB-435 cells NUHoepAxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGrt[ZA1QCCq NV\GNYx1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUCuOFgh|ryP M{\ZTlI1OTF7NUW1
OVCAR5 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 NXLvNo1tPDhiaB?= MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME2wMlYyKM7:TR?= M{DYc|I1OTF7NUW1

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Administration of SB939 (25 mg/kg to 100 mg/kg) displays a dose-dependent antitumor efficacy in a xenograft mice model of human colorectal cancer (HCT-116). This is approximately twice as efficacious as SAHA: SB939 causing a tumor growth inhibition of 94% versus 48% by SAHA with both at the maximum tolerated dose. Oral administration of SB939 at a dose of 50 mg/kg or 75 mg/kg in the APCmin genetic mice model of early-stage colon cancer markedly reduces the number of tumors , decreases cumulative hemocult scores and increases hematocrit values more effectively than 5-fluorouracil. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

HDAC enzyme assay:

All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software.
細胞試験: [1]
+ 展開
  • 細胞株: HCT116, A2780, ACHN, MCF7, HL-60, et al.
  • 濃度: Dissolved in DMSO (stock concentration, 10 mM), final concentrations 1.5 nM to 100 μM
  • 反応時間: 96 hours
  • 実験の流れ: Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: BALB/c nude mice bearing HCT-116 human colon cancer xenografts, Male and APCmin mice
  • 製剤: Dissolved in DMSO and prepared in 0.5% methylcellulose (w/v) and 0.1% Tween-80 in water
  • 投薬量: 25, 50, 75, or 100 mg/kg
  • 投与方法: Oral gavage once daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 72 mg/mL (200.84 mM)
Ethanol 27 mg/mL (75.31 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
1% DMSO+30% polyethylene glycol+1% Tween 80
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 358.48
化学式

C20H30N4O2

CAS No. 929016-96-6
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03495934 Enrolling by invitation Healthy Subjects Helsinn Healthcare SA|Quotient Sciences February 8 2018 Phase 1
NCT03151304 Recruiting Myelodysplastic Syndromes Helsinn Healthcare SA June 1 2017 Phase 2
NCT03151408 Recruiting Acute Myeloid Leukemia Helsinn Healthcare SA|Clinipace Worldwide June 23 2017 Phase 3
NCT02267278 Completed Myeloproliferative Diseases M.D. Anderson Cancer Center|Helsinn Healthcare SA January 12 2015 Phase 2
NCT02118909 Completed Healthy Volunteers|Non-smokers Helsinn Healthcare SA May 2014 Phase 1
NCT02058784 Completed Healthy Volunteers|Moderate to Heavy Smokers|Non-smokers Helsinn Healthcare SA|Celerion February 2014 Early Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HDACシグナル伝達経路

HDAC Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID